Presentation Outline ICHP Annual Meeting September 13-15

Protease Inhibitors
• Require “boosting” with ritonavir
Darunavir/r = Atazanavir/r > lopinavir/r
All other PIs
ARTEMIS: DRV/RTV vs LPV/RTV in Treatment‐
Naive Patients
• Randomized, open‐label phase III study
• Primary endpoint: HIV‐1 RNA < 50 copies/mL at Week 48
Antiretroviral-naive patients
(N = 689)
Week 48 primary endpoint [1] Week 96 [
DRV/RTV 800/100 mg QD
+ TDF/FTC
(n = 343)
LPV/RTV 400/100 mg BID or 800/200 mg QD*
+ TDF/FTC
(n = 346)
*Dosing based on regulatory approval; 77% of patients received BID dosing.
ARTEMIS: Wk 96 Lipid Substudy
• Statistically greater % increases in
TC, TG in LPV/RTV arm than
DRV/RTV arm (P < .001)
Median Increase at Wk W 96 (mg/dL)
60
50
40
30 26
20
10
0
35
17 15
DRV/RTV
LPV/RTV
TC LDL-C HDL-C TG
5
8
18
56
Plasma Conceentration
Boosting PI Levels With ritonavir
Moyle G, et al. Drugs. 1996;51:701-712.
Time
boosted PI
ARTEMIS: Week 48 and 96 Response
PI toxicity
threshold
PI level required
to overcome
“resistant” virus
PI PI level required to
overcome WT virus
48 weeks non‐inferior, 96 weeks superior‐ this is the first head‐head PI trial in
Tx naïve pts that showed superiority
HIV-1 RNA < 50 copies/mmL
(% [±SE])
100
80
60
40
20
0
0
84%
78%
DRV/RTV (n = 343)
LPV/RTV (n = 346)
8 16 24 36 48
Weeks
60 72 84 96
79%
71%
CASTLE: ATV/RTV vs LPV/RTV in Treatment‐Naive
Patients
• Multicenter, randomized, open‐label phase III study
• Primary endpoint: HIV‐1 RNA < 50 copies/mL at Week 48
Antiretroviral-naive
(N = 883)
ATV/RTV 300/100 mg QD +
TDF/FTC FDC
(n = 440)
LPT/RTV 400/100 mg BID* +
TDF/FTC FDC
(n = 443)
Week 48
8/30/2012
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